Cat. No.: HY-16069

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Tucatinib

(Synonyms: Irbinitinib; ARRY-380; ONT-380)

19 Cited Publications

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Based on 19 publication(s) in Google Scholar

Tucatinib (Irbinitinib) is a potent, orally active and selective HER2 inhibitor with an IC₅₀ of 8 nM.

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Pureté: 99.48%
CAS No.: 937263-43-9
Formule: C₂₆H₂₄N₈O₂
Masse moléculaire:480.52

Stockage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Tucatinib Chemical Structure

CAS No.: 937263-43-9

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Activité biologique
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
- Essai clinique
Chemical Information
Publications (19)
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références
Help & FAQs
Bioz

Activité biologique

Description

Tucatinib (Irbinitinib) is a potent, orally active and selective HER2 inhibitor with an IC₅₀ of 8 nM.

IC₅₀ & Target

HER2

Voir tous les produits spécifiques à Isoform EGFR :

In Vitro

Tucatinib has nanomolar activity against purified HER2 enzyme and is approximately 500-fold selective for HER2 versus EGFR in cell-based assays. Tucatinib selectively inhibits the receptor tyrosine kinase HER2 relative to EGFR^[1].
Tucatinib blocks proliferation and the phosphorylation of HER2 and its downstream effector, Akt in HER2 overexpressing cell lines. In the EGFR overexpressing cell lines, it weakly inhibits phosphorylation and proliferation, demonstrating that Tucatinib may have potential to block HER2 signaling without causing the toxicities of EGFR inhibition^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Tucatinib (ONT-380, 200 mg/kg/d) shows a survival benefit when each drug is dosed at the maximum-tolerated dose^[1].
Tucatinib and its active metabolite causes a significant reduction in brain pErbB2 (80%)^[2].
Tucatinib (ARRY-380) demonstrates significant dose-related tumor growth inhibition (TGI; 50% at 50 mg/kg/d and 96% at 100 mg/kg/d) with numerous partial regressions (>50% reduction from baseline size) at the higher dose level in 9/12 animals. Tucatinib (50 mg/kg/d) in combination with trastuzumab shows a 98% TGI with complete regressions in 9/12 animals and two partial regressions^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

Female nude mice^[3].
Dosage:

200 mg/kg/d.
Administration:

PO, daily.
Result:

Exhibited anti-tumor activity and benefited survival.

Essai clinique

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 937263-43-9
Appearance Solid
Masse moléculaire 480.52
Formule C₂₆H₂₄N₈O₂
Color White to yellow
SMILES

CC1=CC(NC2=C3C=C(NC4=NC(C)(C)CO4)C=CC3=NC=N2)=CC=C1OC5=CC6=NC=NN6C=C5
Synonyms

Irbinitinib; ARRY-380; ONT-380
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (19)

All Cell Proliferation/Viability AssayBio/Physico-chemical Assay

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Journal Impact Factor

Cancer Discov

Ontogeny and Vulnerabilities of Drug-Tolerant Persisters in HER2+ Breast Cancer. [Abstract]

2022 Apr 1;12(4):1022-1045. PMID: 34911733

Tucatinib purchased from MedChemExpress. Usage Cited in: Cancer Discov. 2022 Apr 1;12(4):1022-1045. [Abstract]

HER2+ breast cancer cell lines were treated with 1.2 μM Tucatinib (0-49 days), counted at the indicated times, and the percentage of the initial cell number was determined.

Tucatinib purchased from MedChemExpress. Usage Cited in: Cancer Discov. 2022 Apr 1;12(4):1022-1045. [Abstract]

GSEA shows enrichment of “Hallmark Epithelial Mesenchymal Transition” genes in mesenchymal-like DTPs (top) and “Hallmark Estrogen Responses Early” in luminal-like DTPs (bottom) evoked by Tucatinib.

Tucatinib purchased from MedChemExpress. Usage Cited in: Cancer Discov. 2022 Apr 1;12(4):1022-1045. [Abstract]

Heatmaps show supervised clustering of Parental, Lapatinib-DTPs and Tucatinib-DTPs with mesenchymal-DTP DEGs (left) or luminal DTP DEGs (right). Scale represents the z-score.
Nat Cancer

The MEK-RAF molecular glue IK-595 has potent antitumor activity across RAS/MAPK pathway-altered cancers. [Abstract]

2026 Jan;7(1):116-130. PMID: 41482524
Cell Host Microbe

Peptostreptococcus stomatis promotes colonic tumorigenesis and receptor tyrosine kinase inhibitor resistance by activating ERBB2-MAPK. [Abstract]

2024 Jul 23:S1931-3128(24)00254-3. PMID: 39059397
Nat Commun

Molecular landscape, subtypes, and therapeutic vulnerabilities of central nervous system solitary fibrous tumors. [Abstract]

2025 Aug 23;16(1):7870. PMID: 40849425

Tucatinib purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Aug 23;16(1):7870. [Abstract]

Heatmap of the inhibitory effect of Ceritinib, Pyrotinib and Tucatinib on 76 tyrosine kinases at a concentration of 1 μM.

Tucatinib purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Aug 23;16(1):7870. [Abstract]

Dose–response curves of primary SFT cells treated with ceritinib, pyrotinib, tucatinib (0-10 μM, 72 h), E260, and DS21360717 (biological replicates n = 3).
Sci Transl Med

PP2A inhibition is a druggable MEK inhibitor resistance mechanism in KRAS-mutant lung cancer cells. [Abstract]

2018 Jul 18;10(450):eaaq1093. PMID: 30021885
Clin Cancer Res

IRX4204 Induces Senescence and Cell Death in HER2-positive Breast Cancer and Synergizes with Anti-HER2 Therapy. [Abstract]

2024 Jun 3;30(11):2558-2570. PMID: 38578278
Acta Pharmacol Sin

CHMFL-26 is a highly potent irreversible HER2 inhibitor for use in the treatment of HER2-positive and HER2-mutant cancers. [Abstract]

2022 Oct;43(10):2678-2686. PMID: 35228653
EMBO Mol Med

PlexinD1 is a driver and a therapeutic target in advanced prostate cancer. [Abstract]

2025 Feb;17(2):336-364. PMID: 39748059
Cell Death Discov

Targeting the up-regulated CNOT3 reverses therapeutic resistance and metastatic progression of EGFR-mutant non-small cell lung cancer. [Abstract]

2023 Nov 2;9(1):406. PMID: 37919290
Mol Oncol

Cellular liquid biopsy provides unique chances for disease monitoring, preclinical model generation and therapy adjustment in rare salivary gland cancer patients. [Abstract]

2025 Jul;19(7):2056-2073. PMID: 39367702
Drug Metab Dispos

Impact of variation in CYP3A and CYP2C8 on tucatinib metabolic clearance in human liver microsomes. [Abstract]

2025 May;53(5):100061. PMID: 40233610
Sci Rep

A degrader of HER2 and EGFR abolishes p95HER2 and shows robust antitumor efficacy in HER2-positive breast cancer. [Abstract]

2026 Apr 20;16(1):12890. PMID: 42009845
Breast Cancer (Dove Med Press)

Therapeutic Advantage of Targeting PRMT5 in Combination with Chemotherapies or EGFR/HER2 Inhibitors in Triple-Negative Breast Cancers. [Abstract]

2023 Nov 6:15:785-799. PMID: 37954171
Dis Model Mech

Fibroblast-derived EGF ligand Neuregulin-1 induces fetal-like reprogramming of the intestinal epithelium without supporting tumorigenic growth. [Abstract]

2023 Apr 1;16(4):dmm049692. PMID: 36912192
Cancer Chemother Pharmacol

UCP-2 inhibitor enhanced the efficacy of trastuzumab against HER2 positive breast cancer cells. [Abstract]

2021 Oct;88(4):633-642. PMID: 34146128
Biomed Chromatogr

Quantitation of Tucatinib, a Novel Tyrosine Kinase Inhibitor in Dried Blood Spot (DBS) With LC-ESI-MS/MS: Application to a Pharmacokinetic Study in Mice. [Abstract]

2026 Aug;40(8):e70527. PMID: 42328931
bioRxiv

2026 Jun 19.
bioRxiv

Protein-ligand binding kinetics are primarily controlled by the protein, not the ligand. [Abstract]

2026 May 22:2026.05.20.726507. PMID: 42239232
Complutense University of Madrid

2025.

Solvant et solubilité

In Vitro:

DMSO : 41.67 mg/mL (86.72 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.0811 mL

10.4054 mL

20.8108 mL

5 mM

0.4162 mL

2.0811 mL

4.1622 mL

10 mM

0.2081 mL

1.0405 mL

2.0811 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Calculateur de molarité

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 5% DMSO 40% PEG300 5% Tween-80 50% Saline

Solubility: ≥ 2.62 mg/mL (5.45 mM); Clear solution

Protocol 2

Add each solvent one by one: 5% DMSO 95% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.62 mg/mL (5.45 mM); Clear solution

Protocol 3

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: 2.08 mg/mL (4.33 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 4

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: 2.08 mg/mL (4.33 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 5

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.08 mg/mL (4.33 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

Working Solution

For the following dissolution methods, please prepare the working solution directly:

It is recommended to prepare fresh solutions and use them promptly within a short period of time.

The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 30% SBE-β-CD in Saline

Solubility: 10 mg/mL (20.81 mM); Suspension solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (283 KB)
SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Portuguese - PT (396 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[1]. Moulder-Thompson S, et al. Phase 1 Study of ONT-380, a HER2 Inhibitor, in Patients with HER2⁺ Advanced Solid Tumors, with an Expansion Cohort in HER2+ Metastatic Breast Cancer (MBC). Clin Cancer Res. 2017 Jan 4. pii: clincanres.1496.2016. [Content Brief]

[2]. Abstract: In: Proceedings of the 103rd Annual Meeting of the American Association for Cancer Research; 2012 Mar 31-Apr 4; Chicago, IL. Philadelphia (PA): AACR; Cancer Res 2012;72(8 Suppl):Abstract nr 852. doi:1538-7445.AM2012-852

[3]. P. Lee, et al. In Vivo Activity of ARRY-380, a Potent, Small Molecule Inhibitor of ErbB2 in Combination with RP-56976. Cancer Research

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.0811 mL	10.4054 mL	20.8108 mL	52.0270 mL
	5 mM	0.4162 mL	2.0811 mL	4.1622 mL	10.4054 mL
	10 mM	0.2081 mL	1.0405 mL	2.0811 mL	5.2027 mL
	15 mM	0.1387 mL	0.6937 mL	1.3874 mL	3.4685 mL
	20 mM	0.1041 mL	0.5203 mL	1.0405 mL	2.6013 mL
	25 mM	0.0832 mL	0.4162 mL	0.8324 mL	2.0811 mL
	30 mM	0.0694 mL	0.3468 mL	0.6937 mL	1.7342 mL
	40 mM	0.0520 mL	0.2601 mL	0.5203 mL	1.3007 mL
	50 mM	0.0416 mL	0.2081 mL	0.4162 mL	1.0405 mL
	60 mM	0.0347 mL	0.1734 mL	0.3468 mL	0.8671 mL
	80 mM	0.0260 mL	0.1301 mL	0.2601 mL	0.6503 mL

Keywords

Tucatinib

19 Cited Publications

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Tucatinib

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Publications Citing Use of MedChemExpress (MCE) Tucatinib

Voir tous les produits spécifiques à Isoform EGFR

Activité biologique

Chemical Information

Publications (19)

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

Tucatinib Related Classifications

Cat. No.: HY-16069